Application of stevioside R1 and its derivative as medicine for preventing and treating neurodegeneration disease

A neurodegenerative and disease-related technology, applied in nervous system diseases, drug combinations, pharmaceutical formulas, etc., can solve problems such as lack of berries, and achieve the effect of reducing damage

Inactive Publication Date: 2005-04-27
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Method used

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  • Application of stevioside R1 and its derivative as medicine for preventing and treating neurodegeneration disease
  • Application of stevioside R1 and its derivative as medicine for preventing and treating neurodegeneration disease
  • Application of stevioside R1 and its derivative as medicine for preventing and treating neurodegeneration disease

Examples

Experimental program
Comparison scheme
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Embodiment 1

[0022] Embodiment 1. Extraction of sweet leaf glycoside R1 (Suavissimoside R1)

[0023] We use the whole plant of Rubus parvifollus L in the Rosaceae family, use its dry powder, and extract it with ethanol for several times, and recover ethanol from the extract. The residue was suspended in water with petroleum ether to remove fat-soluble components, extracted with ethyl acetate, the extract was dissolved in methanol and mixed with silica gel, passed through a chromatography column, and eluted with petroleum ether: ethyl acetate gradient to obtain colorless needle crystals sexual component. We found that this ingredient is easily soluble in methanol, ethanol, alkaline aqueous solution and other solvents; soluble in ethyl acetate, acetone and other solvents; slightly soluble in water; insoluble in chloroform, petroleum ether, ether, dichloromethane and other solvents. According to the above extraction method, the yield is about 1‰, and the component turns blue when heated with...

Embodiment 2

[0024] Example 2. Effect of Rubioside R1 on MPTP-Induced Parkinson's Disease Animals

[0025] 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, MPTP) is a white powder neurotoxin , can specifically destroy dopaminergic nerve cells, thereby damaging the nigrostriatal pathway in the brain, causing symptoms similar to Parkinson's disease in humans and animals. MPTP was made into the required concentration with physiological saline.

[0026] Referring to the experimental method of Tatton et al. (Neuroscience, 1997; 77: 1037-1048), 60 male C57BL type black mice were selected and randomly divided into normal saline (NS) group, MPTP (M) group and steroside R1+MPTP (CH ) three dose groups, 20 rats in each group. On the first day of the experiment, the CH group was given 1, 3, and 10 mg kg of glucoside R1, respectively. On the second day, the CH group was administrated with glucoside R1 (the same dose as the first day), and 30 minutes later, ...

Embodiment 4

[0047] Example 4. 6-hydroxydopa (6-OHDA)-induced Parkinson's disease model

[0048] Male Wistar rats, 200~250g. After intraperitoneal injection of pentobarbital sodium (45mg / kg) anesthesia, fix it on the stereotaxic instrument, and inject the newly prepared and cooled 6-OHDA normal saline solution (2mg / ml, containing ascorbic acid 0.2mg / ml) at two points on the right side. ml), damage the midbrain striatal pathway. First point: tooth bar=-2.4mm, A=-4.4mm, L=+1.2mm (right side), V=+7.8mm (depth), inject 3 μl. Second point: tooth bar=+3.4mm, A=-4.0mm, L=+0.75mm (right side), V=8.0mm (depth), inject 3 μl. The needle was retained for 3 minutes, and the same solute control injection without drug was performed in the contralateral brain region. One week after the operation, APO 0.5mg / kg was injected subcutaneously to induce it to rotate to the left, and the number of rotations of the rat was observed every 5 minutes, 1 minute each time, and recorded for 40 minutes in total. The ...

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Abstract

Japanese raspberry herb, Stevioside R1 and its derivative are used in preparing medicine for preventing and treating neurodegeneration disease. Animal and human body experiments show that the medicine has excellent treating effect on neurodegeneration diseases, including Parkinson's disease, senile dementia, etc. with high treating index and high safety.

Description

technical field [0001] The present invention relates to the application of sweet leaf glycoside R1 and derivatives thereof as medicines for preventing and treating neurodegenerative diseases. Background technique [0002] Neurodegenerative diseases refer to a series of diseases caused by degenerative changes of neurons in the human body, which mostly occur in the elderly and greatly affect people's quality of life, such as Parkinson's disease (PD) and senile dementia Alzheimer's disease (AD) is two neurodegenerative diseases with high incidence; other neurodegenerative diseases include amyotrophic lateral sclerosis (ALS), neurofibromatosis, Huntington's disease, myoclonic Epilepsy, familial blindness, demyelinating disease, spinal cord injury, etc. Former U.S. President Clinton listed neurodegenerative diseases as one of the urgent tasks facing the medical profession in his debriefing speech before leaving office. [0003] Evidence suggests that neuronal loss resulting fro...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P25/00A61P25/16A61P25/28
Inventor 陈汝筑于占洋
Owner SUN YAT SEN UNIV
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